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Medicinal aerosol formulations

An aerosol and preparation technology, applied in the field of pharmaceutical aerosol preparations, can solve the problems of inaccurate dosage and uneven content

Inactive Publication Date: 2005-07-06
3M INNOVATIVE PROPERTIES CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Precipitation, emulsion stratification or flocculation of the drug can lead to large inhomogeneities in its content, which in turn can lead to inaccurate dosing when the above formulation is administered through the metering valve

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Duration (minutes)

[0033] Microscopic analysis of the product after 40 minutes revealed that it was significantly smaller than 1 micron. The product was measured by scanning electron microscopy (SEM), and its particle size was estimated to be 100 nm. After 5 minutes and 40 minutes in the above scheme, a certain amount of the dispersion (1.5g) was extracted and added to a 20ml clean pressure-resistant plastic bottle, and then a non-quantitative valve was installed at an appropriate position. Then HFA 134a (20g) was injected through each valve. Compared with the preparation of the sample at 5 minutes, the suspension preparation made from the sample at 40 minutes has a significantly lower sedimentation rate and a larger deposition volume. These two characteristics are used as a bulking agent for metered inhalation. Suspension formulations are advantageous. Therefore, a technique has been found to provide a stable suspension of an excipient (lactose) with a typical ...

Embodiment 2

[0035] The slurry formed by micronized lactose monohydrate (15 g) and absolute ethanol was processed according to the method in Example 1.

[0036] The lactose slurry was concentrated by centrifugation at 5000 rpm for 5 minutes, and 10 g was added to each centrifuge tube. After pouring out the excess ethanol, the ratio of lactose to ethanol is 1:4. Add it as a thick paste to the inner wall of a polyethylene terephthalate vial. Micronized formoterol fumarate has been added to the polyethylene terephthalate vial, and then added to the propellant The agent was prepared into the following formulation:

[0037] mg / ml g / unit mg / ml g / unit mg / ml g / unit

[0038] Formote fumarate 0.132 0.0020 0.132 0.0017 0.132 0.0018

[0039] Lactose monohydrate 2.640 0.0390 2.640 0.0340 2.640 0.0357

[0040] Ethanol 12.180 0.1800 13.960 0.1800 13.317 0.1800

[0041] HFA 134a 1203.048 17.7790 0.000 0.0000 493.337 6.6684

[0042] HFA 227 0.000 0.0000 1379.268 17.7843 822.288 11.1141

[0043] ...

Embodiment 3

[0047] A further formulation was prepared in a manner similar to that of Example 2. This preparation used nanoparticulate lactose and micronized lactose, but did not contain drugs, and had the following composition:

[0048] mg / ml g / unit mg / ml g / unit mg / ml g / unit

[0049] Lactose monohydrate 2.772 0.0410 2.772 0.0357 2.772 0.0375

[0050] Ethanol 12.180 0.1800 13.960 0.1800 13.317 0.1800

[0051] HFA 134a 1203.048 17.7790 0.000 0.0000 493.337 6.6684

[0052] HFA 227 0.000 0.0000 1379.268 17.7843 822.228 11.1141

[0053] The results measured by the optical measurement technique are similar to the results of the formulation in Example 2. The sedimentation speed of the samples containing nano-lactose is slower than that of all the samples containing the air-jet pulverized micronized lactose.

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Abstract

The use of a microparticle loosening agent in a pharmaceutical aerosol formulation comprising a suspension of drug particles in a propellant, the microparticle loosening agent having a very small mass median diameter, which is less than 1 micron, preferably less than 300nm. Particulate loosening agents include, for example, vitamin C, sugars, polysaccharides, amino acids, organic and inorganic salts, urea, and propiododon.

Description

Invention field [0001] The invention relates to a medicinal aerosol preparation, in particular to a suspension aerosol preparation containing drug particles and a nanoparticle auxiliary powder, which is suitable for respiratory tract administration. Background of the invention [0002] Medicinal aerosol preparations packed in pressure-resistant containers have been used for more than 40 years. Most of the time, chlorofluorocarbons are used as propellants. The drug is formulated into a solution or suspension according to its dissolution properties and other factors. After recognizing that the use of the above-mentioned propellants had an adverse effect on the environment, other propellants were adopted, which posed a challenge to reformulation or the introduction of new drugs, and also presented an opportunity to provide improved formulation processes. [0003] Two satisfactory propellants have appeared. They are 1,1,1,2-tetrafluoroethane (HFA134a) and 1,1,1,2,3,3,3-heptafluoropro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12A61KA61K9/00A61K9/10A61K9/16A61K31/137A61K31/46A61K31/56A61K47/00A61K47/04A61K47/10A61K47/12A61K47/14A61K47/16A61K47/18A61K47/22A61K47/26A61K47/36A61P11/00A61P11/08
CPCA61K9/0075A61K9/008A61P11/00A61P11/06A61P11/08
Inventor 菲利浦·A·因克斯莱斯莉·麦肯齐詹姆斯·T·利斯特
Owner 3M INNOVATIVE PROPERTIES CO
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